Target Information

Target General Infomation
Target ID
T97917
Former ID
TTDR00540
Target Name
FMLP-related receptor I
Gene Name
FPR2
Synonyms
FMLP-R-I; FPRL1; Formyl peptide receptor-like 1; G-protein-coupled receptor FPR-Like-1; HM63; LXA4 receptor; Lipoxin A4 receptor; RFP; FPR2
Target Type
Research
Function
Low affinity receptor for N-formyl-methionyl peptides, which are powerful neutrophils chemotactic factors. Binding of FMLP to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The activation of LXA4R could result in an anti-inflammatory outcome counteracting the actions of proinflammatory signals such as LTB4 (leukotrieneB4).
BioChemical Class
GPCR rhodopsin
UniProt ID
P25090
Sequence
METNFSTPLNEYEEVSYESAGYTVLRILPLVVLGVTFVLGVLGNGLVIWVAGFRMTRTVT
TICYLNLALADFSFTATLPFLIVSMAMGEKWPFGWFLCKLIHIVVDINLFGSVFLIGFIA
LDRCICVLHPVWAQNHRTVSLAMKVIVGPWILALVLTLPVFLFLTTVTIPNGDTYCTFNF
ASWGGTPEERLKVAITMLTARGIIRFVIGFSLPMSIVAICYGLIAAKIHKKGMIKSSRPL
RVLTAVVASFFICWFPFQLVALLGTVWLKEMLFYGKYKIIDILVNPTSSLAFFNSCLNPM
LYVFVGQDFRERLIHSLPTSLERALSEDSAPTNDTAANSASPPAETELQAM
Agonist AG-26 Drug Info [530510]
aspirin triggered lipoxin A4 Drug Info [543579]
aspirin-triggered resolvin D1 Drug Info [531857]
ATLa2 Drug Info [527021]
compound R-(-)-5f Drug Info [531913]
fMet-Leu-Phe Drug Info [533990]
humanin Drug Info [527235]
LXA4 Drug Info [530641]
pyrazolone, 1 Drug Info [528203]
quin-C1 Drug Info [527167]
resolvin D1 Drug Info [530641]
RvD1-ME Drug Info [531857]
[3H]LXA4 Drug Info [526742]
Antagonist compound 1754-31 Drug Info [532404]
quin-C7 Drug Info [528957]
Pathways
Pathway Interaction Database Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
Reactome G alpha (q) signalling events
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 526742Lipoxin recognition sites. Specific binding of labeled lipoxin A4 with human neutrophils. J Biol Chem. 1992 Aug 15;267(23):16168-76.
Ref 527021Novel 3-oxa lipoxin A4 analogues with enhanced chemical and metabolic stability have anti-inflammatory activity in vivo. J Med Chem. 2004 Apr 8;47(8):2157-65.
Ref 527167A novel nonpeptide ligand for formyl peptide receptor-like 1. Mol Pharmacol. 2004 Nov;66(5):1213-22. Epub 2004 Aug 12.
Ref 527235N-Formylated humanin activates both formyl peptide receptor-like 1 and 2. Biochem Biophys Res Commun. 2004 Nov 5;324(1):255-61.
Ref 528203Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3713-8. Epub 2006 May 11.
Ref 528957Pharmacological characterization of a novel nonpeptide antagonist for formyl peptide receptor-like 1. Mol Pharmacol. 2007 Oct;72(4):976-83. Epub 2007 Jul 25.
Ref 530510Identification of novel small-molecule agonists for human formyl peptide receptors and pharmacophore models of their recognition. Mol Pharmacol. 2010 Feb;77(2):159-70.
Ref 530641Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc Natl Acad Sci U S A. 2010 Jan 26;107(4):1660-5.
Ref 531857Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs. Am J Pathol. 2012 May;180(5):2018-27.
Ref 531913Synthesis, enantioresolution, and activity profile of chiral 6-methyl-2,4-disubstituted pyridazin-3(2H)-ones as potent N-formyl peptide receptor agonists. Bioorg Med Chem. 2012 Jun 15;20(12):3781-92.
Ref 532404Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries. Mol Pharmacol. 2013 Sep;84(3):314-24.
Ref 533990Multiple domains of the N-formyl peptide receptor are required for high-affinity ligand binding. Construction and analysis of chimeric N-formyl peptide receptors. J Biol Chem. 1993 Aug 25;268(24):18167-75.
Ref 543579(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 223).

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